For research use only
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GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.
|IC50 & Target|
IC50: 2.5 nM (MMP9), 5.3 nM (ADAM10)
In cellular assay 25 µM and even a concentration of 1 µM GI254023X strongly reduces constitutive RAGE shedding; also PACAP-inducing shedding of RAGE is significantly reduced. At a concentration of 100 nM, a slight inhibition of RAGE shedding is still observed. In in vitro assays with recombinant proteinases, GI254023X discriminates between ADAM17 (IC50=541 nM) and ADAM10 (IC50=5.3 nM)/MMP9 (IC50=2.5 nM). CXCL16 shedding is inhibited by ADAM protease inhibitors (e.g GI254023x). A2780 cells are incubated with the ADAM-10/ADAM-17 inhibitor TAPI-2, as well as the ADAM-10-selective inhibitor GI254023x, as the level of expressed ADAM-10 is on average 9.8-fold higher on mRNA level compare with ADAM-17. In addition, GI254023x also prevents CXCL16 shedding from the cell membrane and is even more potent than TAPI-2. When apply the specific ADAM10 (α-secretase) inhibitor GI254023X (5 mM) to serum/glucose-deprived slices, PI counts are significantly increased in comparison with DMSO (carrier)-treated controls.
|In solvent||-80°C||6 months|
. M J M Gooden, et al. Elevated serum CXCL16 is an independent predictor of poor survival in ovarian cancer and may reflect pro-metastatic ADAM protease activity. British Journal of Cancer (2014) 110, 1535–1544.